Etamicastat hydrochloride|677773-32-9|(BIA 5-453 hydrochloride)-陌孚医药/Medlife

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Etamicastat hydrochloride (Synonyms: BIA 5-453 hydrochloride)

目录号: PL13547 纯度: ≥98%

Etamicastat hydrochloride (BIA 5-453 hydrochloride) 是一种有效且可逆的多巴胺 β-羟化酶 (DBH) 抑制剂，IC50 值为 107 nM。可用于心血管疾病的研究。

CAS No. :677773-32-9

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中文名称	Etamicastat hydrochloride
中文别名	依他米司特盐酸盐
英文名称	Etamicastat hydrochloride
英文别名	Etamicastat HCl;Etamicastat (hydrochloride);(R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydro-2H-imidazole-2-thione hydrochloride;(R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione hydrochloride;(R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1H-imidazole-2(3H)-thione hydrochloride;Etamicastat hydrochloride;E77325;2-[3-[(3R)-6,8-Difluoro-3,4-dihydro-2H-chromen-3
Cas No.	677773-32-9
分子式	C₁₄H₁₆ClF₂N₃Os
分子量	347.81
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

Etamicastat hydrochloride (BIA 5-453 hydrochloride) 是一种有效且可逆的多巴胺 β-羟化酶 (DBH) 抑制剂，IC₅₀ 值为 107 nM。可用于心血管疾病的研究。

生物活性

Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC 50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.

性状

Solid

IC50 & Target[1][2]

IC50: 107 nM (DBH)

体外研究(In Vitro)

Etamicastat blocks the hERG current amplitude with an IC50 value of 44 μg/mL (141 μM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Etamicastat (100 mg/kg; administered intraperitoneally) leads to a significant reduction of noradrenaline levels in heart with concomitant increasing in dopamine levels.
Etamicastat (50 mg/kg; a single oral administration) exhibits moderate oral bioavailability (64%), C max (4.9 nM), and terminal elimination half-lives (T 1/2 =3.7 h) in male Wistar rats.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Loureiro AI, et al. Etamicastat, a new dopamine-?-hydroxylase inhibitor, pharmacodynamics and metabolism in rat. Eur J Pharmacol. 2014 Oct 5;740:285-94.
[2]. ManuelVaz-da-Silva, et al. Cardiac safety profile of etamicastat, a novel peripheral selective dopamine-β-hydroxylase inhibitor in non-human primates, human young and elderly healthy volunteers and hypertensive patients. IJC Metabolic & Endocrine. 2015 Ju

溶解度数据	In Vitro: DMSO : 100 mg/mL (287.51 mM; Need ultrasonic)H₂O : 16.67 mg/mL (47.93 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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